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Flashcards in Pharm 9.2 Deck (98)
1

Epinephrnien on SM in GIT

relaxation, peristalsis is reduced and sphincters are constricted

2

Epi on SM in Bladder

trigone and sphincter contricted (alpha 1 rec), detrusor relaxed (beta 2), net effect is urinary retentino

3

Epi on SM in uterus

relaxation at term (tocolysis - lysis of contraction of the uterus so no risk of premature delivery)

4

dialation of puple

alpha 1 agonist on radial muscles

5

constriction of pupil

M3 muscaranic agonis on sphincter pupallae

6

uses of Epinephrine

bronchospasm, anaphylactic shock, local anaesthetics, glaucoma, cardiact arrest

7

Epi in bronchospasm

primary drug used in emergency due to acute attacks of asthma

8

Epi in anaphylactic shock

drug of choice, can increase BP in deadly hypotension and increase respiratory exchange

9

what is the durg of choice in anaphylactic shock

epinephrine

10

epi with local anaesthetics (adjunct)

1/100, 000 parts, increase duration of action of local anaesthetic due to alpha 1 and beta 2 effects (low dose beta 2) (Epinephrine + Lidocain)

11

epi with glaucoma (open angle)

decrease IOT due to decreased production of aqueous humor by vasoconstriction of ciliary body blood vessels (2% eyedrop)

12

Prodrug for glaucoma

Dipivefrin - rarely used

13

epi with cardiac arrest

to restore cardiac rhythm in patients with cardiac arrest or heart block regardless of cause

14

Epinephrine adverse effects

palpitation, restlessness, tremors, increase in BP, arrhythmia, cerebral hemorrhage (due to marked elevation of BP)

15

when is epinephrine contraindicated

angina pectoris

16

epinephrine interactions

hypertyroidism, cocaine, diabetes, beta blockers

17

epinephrine, norepinephrine, and dopamine are orally

inactive

18

duration of action of epinephrine

rapid onset but a brief duration of action (due to rapid degradation)

19

epinephrine and norepinephrine are degraded by

MAO and COMT of the intestine wall and liver

20

treat hyperthyroidsm by

using a beta blocker to block the hyper adrenergic state

21

how does cocain affect epinephrine

inhibits its reuptake

22

betablockers given with epinephrine

only left wth alpha 1 effects causing vasoconstriciton

23

Epinephrine can be given

IV, intracardiac, inhalational, subcutaniously, endotracheal tube, or topically

24

Norepinephrine activates

all but BETA 2, more alpha effects causing vasoconstirction, reflex bradycardia

25

NE on TPR

inc TPR due to vasoconstriction of most of the vascular beds

26

NE on systolic and diastolic BP

increase

27

NE on pulse rate

decrease pulse rate (reflex bradycardia) due to inc in BP, reflex rise in vagal activity by stimulating barroreceptors, decrease heart rate, decrease pulse rate

28

If atropine is given before NE

it will result in tachycardia

29

NE on alpha 1 receptors

inc TPR, inc BP (potential reflex bradycardia)

30

NE on beta 1 receptors

inc HR, inc SV, inc CO, inc pulse pressure

31

Difference btw high does epinephrine vs NE in reversing hypertension

if you are to use an alpha 1 blocker to reduce vasoconstirctin, epinephrine continues to work on beta 2 receptors that results in hypotension, but NE do not work on beta 2 receptors

32

Isoproterenol

direct acting synthetic catecholamine, nonselective beta agonist

33

isoproterenol on beta 1 receptors

increased contractility and heart rate

34

isoproterenol on beta 2 receptors on heart

decrease in TPR, decrease in mean BP

35

isoproterenol overall effect on heart

systolic blood pressure does not fall significantly as diastolic due to beta 1 receptor action so the pulse pressure decreases

36

activation of beta 2 in the lungs and GI and uterus

relaxation of SM

37

Isoproterenol is used in

bronchospasm, heart block, bradyarrhythmias

38

dopamine acts on

D1, D2, alpha, and beta receptors

39

D1 in the renal and mesenteric blood vesses

dialates - most sensitive at low dose

40

moderate high dose dopamine

positive iontropic action on the heart by beta 1

41

high dose dopamine

vasoconstriction on alpha 1 receptors

42

as the dose increases the binding of dopamine follows

D1 --> beta 1--> alpha 1

43

the shape of the dose response for natriuresis curve of dopamin is

an inverted U

44

natrieurisis and dopamine

both natriuretic and diuretic

45

dopamine increases

myocardial contractility, RBF, GFR, sodium excretion, urine output

46

Dopamine in cardiogenic shock is the drug of choice bc

increases BP by stimulating heart (beta 1), increasing perfusion to kidney and splanchnic areas (through D1 receptors) by vasodialation, increases blood flow to the kidney, increases GFR, increases Na+ diuresis, prevents kidney shutdown

47

Dopamine agonists

fenoldopam, dopexamine

48

dobutamine is a

selective beta1 agonsit, increases the force of contraction of the heart, with little change in HR,

49

why is do butamine a major advantage over other sympathomimetic drugs

used in CCF, MI with failure bc it increases CO without elevating the oxygen demand of myocardium - am major advantage over other sympathomimetic drugs (which work at the expense of oxygen)

50

alpha 1 selective agonists

phenylephrine, methoxamine

51

Phenylephrine is a

specific alpha 1 agonist direct acting noncatecholamine, increases the mean blood pressure viea basoconstriction with minimal effect on pulse pressure, increasein BP can elicit reflex bradycardia, no direct effect on heart

52

Phenylephrine is used in

nasal decongestion, mydriasis, to retard absorption of local anesthetics, to raise BP and to terminate episodes of supraventricular tachycardia (esp Methoxamine)

53

alpha 2 selective agonists

clonidine, methyldopa

54

clonidine is a

alpha 2 selective agonist

55

clonidine acts centrally to produce

inhibition of sympathetic vasomotr centers, decreaseing sympathetic outflow to the periphery

56

clonidine bioavailability

excellent (transdermal patches also available)

57

Clonidien adverse effects

dry mouth, sedation, bradycardia, sexual dysfunction, rebound hypertension (following abrupt withdrawal of clonidine)

58

uses of clonidine

used in hypertension (to lower BP because of its central actions), also used to minimize the symptoms associated with opiates or benzodiazepines withdrawal

59

other alpha 2 agonists

guanfacine, guanabenz, methyldopa (HTN in pregnancy), Tizanidine (spasmolytic)

60

Methyldopa is used for

hypertention in pregnancy

61

Tizanidine is used as a

spasmolytic

62

topical direct acting sympathomimetics

naphazoline, oxymetazoline, xylometazoline

63

Naphazoline is used as

a topical vasoconstrictor - nasal decongestant

64

Oxymetazoline is used to

reduce congestion and swelling of th nasal mucosa - nasal decongestant

65

xylometazoline is used as a

nasal decongestant

66

indirect acting sympathomimetci drugs

amphetamine, tyramine, ephedrine (mixed action)

67

amphetamine is a

noncatecholamine sympathomimetic drug

68

amphetamine function

increases the release of NE, dopamine in synaptic spaces

69

Amphetamine is taken

orally

70

Amphetamine and CNS

has prominent CNS stimulatory action, increases alertness, concentration and wok capacity

71

Amphetamine on RAS

activates reticular activating system producing insomnia

72

Amphetamine on CVS

increases BP and HR

73

Therapeutic uses for amphetamine

CNS stimulant in the treating ADHD, Narcolpecy (esp Modafinil, a new amphetamine substitute), Obesity (appetite control/appetite suppression)

74

Tyramine releases

large amounts of stored CA from nerve terminals

75

is Tyramine used clinically

no

76

Tyramine is found in

fermented foods, such as aged/riped chees, meats, chicken liver, pickled or smoked fish such as anchovies or herrings, and red wines

77

Tyramine is inactivated by

MAO in the gut

78

Tyramine can participate in

the "cheese reaction"

79

Cocain use

local anesthetic agent, having ability to block uptake of NE in the adrenergic neurons; concequently NE accumulates in the synaptic space resulting in enhancement of sympathtic activity. Also a CNS stimulant and drug of abuse.

80

Mixed acting drugs

ephedrine, pseudoephedrine

81

Ephedrine/pseudoephedrine is an

alkaloid from the plant Ephedra vulgaris

82

repeated injections of ephedrine produce

tachyphylaxis

83

Ephedrine is resistnat to

MAO and COMT

84

Ephedrine is effective taken

orally and crosses the BBB - CNS stimulation

85

Ephedrine uses

bronhial asthma (not really no) and nasal congestion

86

Phenylpropanolamine is an

alpha agonist

87

Phenylpropanolamine is used as a

nasal decongestant, may cause severe hypertension

88

Phenylpropanolamine is unsafe because

it causes strokes in women

89

Drugs having selective beta 2 action

albuterol, pirbuterol, salmeterol, foroterol, terbulatine, metaproterenol

90

Tocolytic agents

Ritodrine, Terbutaline (beta 2 agonist)

91

Tocolytic agents work by

relaxing the pregnant uterus and supressing premature labor

92

chart on 108

look at it, mostly tells you cateholamines have no oral activity, but other sympathomemetics do except pehnylephrine and cocaine and the sympathomimetics take hours to work, while catecholamines take minutes

93

Pressor agents

NE, Dopamine

94

Cardiac stimulants

Epinephrine, Isoproterenol, Dobutamine

95

Bronchodialators

Epinephrine, Isoproterenol, Albuterol

96

Nasal decongestants

Ephedrine, Pseudoephedrine, Phenylpropanolamine, Oxymetazoline, Xylometazoline

97

CNS Stimulants

Amphetamine, Ephedrine

98

Uterine relaxants

Isoxsuprine, Terbutaline, Ritodrine